tiospirone [Ligand Id: 101] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL35057 (BMY-13859, Tiospirone) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | B | 8.67 | pKi | 2.14 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
| ChEMBL | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
| ChEMBL | Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (1991) 34: 1068-1072 [PMID:1672156] |
| ChEMBL | Binding affinity against Dopamine receptor D2 receptor of rat corpus striatal tissue with [3H]spiperone | B | 8.08 | pIC50 | 8.4 | nM | IC50 | J Med Chem (1991) 34: 3316-3328 [PMID:1683407] |
| 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 8.3 | pKi | - | - | - | Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (1991) 34: 1068-1072 [PMID:1672156] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor of rat hippocampal tissue with [3H]8-OH-DPAT | B | 8.55 | pIC50 | 2.85 | nM | IC50 | J Med Chem (1991) 34: 3316-3328 [PMID:1683407] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor | B | 9.24 | pKi | 0.58 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
| ChEMBL | Binding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligand | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (1991) 34: 3316-3328 [PMID:1683407] |
| 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 8.3 | pKi | - | - | - | J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983] |
| 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - | J Neurochem (1996) 66: 47-56 [PMID:8522988] |
| 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| GtoPdb | - | - | 7.1 | pKi | - | - | - | J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055] |
| 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| GtoPdb | - | - | 9.2 | pKi | - | - | - | J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
